7442. Pinazepam

Nomenclature

CAS number: 52463-83-9
7-Chloro-1,3-dihydro-5-phenyl-1-(2-propynyl)-2H-1,4-benzodiazepin-2-one; 7-chloro-1-propargyl-5-phenyl-3H-1,4-benzodiazepin-2(1H)-one; Z-905; Domar (Zambeletti); Duna (Tedec Zambeletti).
C18H13ClN2O; mol wt 308.76.
C 70.02%, H 4.24%, Cl 11.48%, N 9.07%, O 5.18%.

Description and references

Prepn: F. Tenconi et al., DE 2339790 (1974 to Zambeletti), C.A. 80, 133492k (1974); C. Podesva, K. Vagi, US 3842094 (1974 to Delmar). Metabolism study: A. Trebbi et al., J. Chromatogr. 110, 309 (1975). Pharmacological and toxicological studies: F. Scrollini et al., Arzneim.-Forsch. 25, 934 (1975). Pharmacokinetics: P. M. Boselli, F. Scrollini, Boll. Chim. Farm. 116, 363 (1977). Psychopharmacological properties: F. Scrollini et al., Arzneim.-Forsch. 28, 423 (1978). Physico-chemical profile: G. Filipi, A Trebbi, Boll. Chim. Farm. 118, 105 (1979). Clinical study: V. Bertoncelli et al., Clin. Ter. 94, 641 (1980).

Chemical structure

Properties

Cryst from methanol/water, mp 140-142°. LD50 in mice, rats (mg/kg): 1355, 5819 orally; 266, 622 i.p. (Scrollini, 1975). Also reported as LD50 in mice (mg/kg): 670 orally (Podesva, Vagi).

Note

This is a controlled substance (depressant): 21 CFR, 1308.14.

Therapeutic Category

Anxiolytic.

Keywords

Anxiolytic; Benzodiazepine Derivatives